Daily Medication Pearl: Tepotinib (Tepmetko) for NSCLC

Tepotinib treats adult patients with metastatic non-small cell lung cancer harboring a mesenchymal epithelial transition exon 14 skipping alteration.

Medication Pearl of the Day: Tepotinib (Tepmetko)

Indication: Tepotinib is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal epithelial transition (MET) exon 14 skipping alteration.

Insight:

  • Dosing: 450 mg orally once daily with food until disease progression or unacceptable toxicity.
  • Dosage forms:Tablets 225 mg.
  • Adverse events (AEs): Most common AEs (≥ 20%) were edema, fatigue, nausea, diarrhea, musculoskeletal pain, and dyspnea. The most common Grade 3 to 4 laboratory abnormalities (≥ 2%) were decreased lymphocytes, decreased albumin, decreased sodium, increased gamma-glutamyltransferase, increased amylase, increased ALT, increased AST, and decreased hemoglobin.
  • Mechanism of action: Tepotinib is a kinase inhibitor that targets MET, including variants with exon 14 skipping alterations. Tepotinib inhibits hepatocyte growth factor-dependent and -independent MET phosphorylation and MET-dependent downstream signaling pathways. Tepotinib also inhibited melatonin 2 and imidazoline 1 receptors at clinically achievable concentrations.
  • Manufacturer: EMD Serono

Sources:

  1. tepmetko-pi.pdf (emdserono.com)
  2. tepmetko image - Google Search